发明名称 |
N-(substituted-methyl)-azetidin-2-ones |
摘要 |
N-Mono or N-disubstituted methyl-2-azetidinones are provided via cyclization of beta -hydroxy or beta -halo substituted acid sec-amides wherein the amide nitrogen is substituted with a mono- or di-substituted methyl group having activating substituents. Cyclization of beta -hydroxy acid amides is mediated by triphenylphosphine-dialkylazodicarboxylate while cyclization of beta -halo acid amides is mediated by strong bases e.g. lithium dialkylamides. E.g. Diethyl amino-protected L-serylaminomalonate is cyclized with 200 mole % TPP-diisopropylazodicarboxylate to N-(diethoxycarbonylmethyl)-3-protected-amino-2-azetidinone. The 2-azetidinones provided are useful intermediates.
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申请公布号 |
US4595532(A) |
申请公布日期 |
1986.06.17 |
申请号 |
US19850718127 |
申请日期 |
1985.04.01 |
申请人 |
UNIVERSITY OF NOTRE DAME DU LAC |
发明人 |
MILLER, MARVIN J. |
分类号 |
C07D205/08;C07D205/085;C07D207/26;C07D207/277;C07D403/04;C07D413/04;(IPC1-7):C07D205/08;C07D401/12 |
主分类号 |
C07D205/08 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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